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Nitro imidazole xanthogenate complex marked by TcO, preparation method and applications

A technology of nitroimidazoles and xanthates, which is applied in the field of radiopharmaceutical chemistry and clinical nuclear medicine, and can solve problems such as limited application and difficulty in measuring tissue oxygen concentration

Inactive Publication Date: 2009-10-14
BEIJING NORMAL UNIVERSITY +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Due to the difficulty of measuring tissue oxygen concentration in vivo in the past, its clinical application is limited.

Method used

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  • Nitro imidazole xanthogenate complex marked by TcO, preparation method and applications
  • Nitro imidazole xanthogenate complex marked by TcO, preparation method and applications
  • Nitro imidazole xanthogenate complex marked by TcO, preparation method and applications

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Embodiment

[0055] Describe the present invention in detail below by embodiment, a kind of 99 Tc m O nuclear-labeled nitroimidazole xanthate complexes:

[0056] (1) Synthesis of Ligand NMXT

[0057] a. Ligand EtNMXT synthesis

[0058] first step:

[0059] Weigh 1.073g of 4-nitroimidazole, 1.073g of 2-bromoethanol and 1.575g of anhydrous potassium carbonate in a 100mL round bottom flask, add 50mL of acetonitrile and mix well, heat to reflux for 4h, cool and filter. After distilling off acetonitrile under reduced pressure, the obtained light yellow oil was washed with acetone, filtered again, and spin-dried to obtain a light yellow oil. Infrared Spectrum: (IR) / cm -1 :vOH:3395,vCH 2 : 2946, vNO 2 : 1536, 1380. NMR spectrum: ( 1 H NMR, D 2 O): δ8.11(s, 1H, CH), δ7,65(s, 1H, CH), δ4.14-4.12(t, 2H, CH 2 ), δ3.80(t, 2H, CH 2 ).

[0060] Step two:

[0061] Weigh 500 mg of the reaction product of the first step, wash with acetone, and filter to obtain a filtrate. Add 720 mg of sodiu...

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Abstract

The invention discloses a nitro imidazole xanthogenate complex marked by TcO with the formula of TcO (NMXT)2; in the formula, NMXT represents a compound containing nitro imidazole xanthogenate. The complex adopts Tc(V)O as a central nucleus and has a geometric configuration with the shape of an irregular square pyramid, wherein O atom in Tc=O bond is positioned at the top point and four sulphur atoms provided by two xanthogenate ligand molecules are positioned at the four points of the bottom surface. By the technical steps of synthesis of ligand NMXT and preparation of TcO (NMXT)2 complex, the TcO (NMXT)2 complex is obtained. The nitro imidazole xanthogenate complex has high radiochemical purity and good stability, has higher uptake value and good detention through in tumor and higher ratio of tumor / muscle, is widely applied to tumor imaging of human body and animal organs and is a novel tumor hypoxia imaging agent which is conveniently promoted and applied.

Description

Technical field [0001] The present invention relates to 99 Tc m O the field of radiopharmaceutical chemistry and clinical nuclear medicine technology for nuclear labeling, especially as it relates to a 99 Tc m O nucleus-labeled nitroimidazole xanthate complex, preparation method and application. Background technique [0002] Tissue hypoxia is a common pathological change in many clinical diseases, which means that the oxygen concentration of the tissue is between normal and anaerobic, and the function is abnormal, but there is no obvious morphological change. In solid tumors, most tumors grow quite rapidly, and the growth rate of blood vessels cannot meet the growth of the tumor, resulting in a serious shortage of blood supply, resulting in hypoxia in the tumor. The reduction of oxygen concentration in tumor tissue can lead to its resistance to radiotherapy and chemotherapy, so the measurement of tissue hypoxia level has become the focus of research. Due to the difficul...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D233/94C07F13/00A61K51/04A61K103/10
Inventor 张俊波任佳蕾林潇王学斌唐志刚张现忠陆洁
Owner BEIJING NORMAL UNIVERSITY
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